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prodrug models

" in MedChemExpress (MCE) Product Catalog:

14

Inhibitors & Agonists

1

Peptides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-162074
    Nipamovir

    		HIV Infection
    Nipamovir is a nitroimidazole prodrug. Nipamovir shows comparable antiviral activity to SAMT-247 (HY-102077) and NS-1040 in both cellular assays and a human ex vivo model of HIV infection, along with low toxicity. Nipamovir has EC50 values of 3.64±3.28 and 3.23±2.81 μM for CEM-SS/HIV-1RF and hPBMC/HIV-192HT599, respectively .
    Nipamovir
  • HY-W811579
    Bensuldazic acid

    		Bacterial Infection
    Bensuldazic acid (compound 4f) is a lipophilic 3,5-disubstituted tetrahydro-2H-1,3,5-thiadiazine-2-thione (THTT) derivative that can be used as a prodrug model. Bensuldazic acid has antifungal activity .
    Bensuldazic acid
  • HY-W811579A
    Bensuldazic acid sodium

    		Bacterial Infection
    Bensuldazic acid sodium (compound 4f) is a lipophilic 3,5-disubstituted tetrahydro-2H-1,3,5-thiadiazine-2-thione (THTT) derivative that can be used as a prodrug model. Bensuldazic acid has antifungal activity .
    Bensuldazic acid sodium
  • HY-168143
    YD1342

    		Histone Methyltransferase Cancer
    YD1342 is a prodrug of YD1130, which exhibits potent inhibitory effects on cellular substrate methylation, breast cancer cell clonogenicity, and tumor growth in animal models, exceeding or matching known PRMT4-specific inhibitors. .
    YD1342
  • HY-149065
    D-685

    		α-synuclein Neurological Disease
    D-685, a prodrug of D-520, exhibits higher in vivo anti-Parkinsonian efficacy in a reserpinized Parkinson's disease (PD) animal model than the parent D-520. D-685 reduces accumulation of human α-synuclein (α-syn) protein. D-685 exhibits facile brain penetration .
    D-685
  • HY-118956
    Adrogolide hydrochloride

    ABT-431 hydrochloride; DAS-431 hydrochloride

    		 Dopamine Receptor Neurological Disease
    Adrogolide hydrochloride (ABT-431 hydrochloride) is a chemically stable prodrug that can convert to the dopamine D1 receptor agonist A-86929. Adrogolide hydrochloride ameliorates the MPTP (HY-15608)-induced Parkinson's Disease in marmoset model, reduces the dyskinesias tendency. Adrogolide hydrochloride reverses Risperidone (HY-11018)-induced cognitive deficits in monkey .
    Adrogolide hydrochloride
  • HY-134521
    Diclofenac amide

    		COX Inflammation/Immunology
    Diclofenac amide is a prodrug for Diclofenac sodium (HY-15037). Diclofenac amide is an orally active inhibitor for COX-1/2, that inhibits the production of prostaglandins (PG) and thromboxanes (TX). Diclofenac amide exhibits anti-inflammatory efficacy in Carrageenan (HY-125474)-induced rat paw edema model without causing gastric ulcer (300 μmol/kg) .
    Diclofenac amide
  • HY-P10759
    DTS-201 sodium

    		Peptide-Drug Conjugate (PDC) Aminopeptidase ADC Cytotoxin Cancer
    DTS-201 sodium (CPI-0004Na) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer .
    DTS-201 sodium
  • HY-161838
    ICT10336

    		ATM/ATR Cancer
    ICT10336 is a hypoxia-responsive prodrug of ATR inhibitor, AZD6738 (HY-19323). ICT10336 is hypoxia-activated and specifically releases AZD6738 only in hypoxic conditions in vitro. This can inhibit ATR activation (T1989 and S428 phosphorylation) and subsequently abrogate HIF1a-mediated adaptation of hypoxic cancers cells, thus selectively inducing cell death in 2D and 3D cancer models. ICT10336 is a metabolic substrate of CYPOR activity.
    ICT10336
  • HY-159925
    QKY-613

    		Cyclic GMP-AMP Synthase
    QKY-613 is a prodrug that enhances immune surveillance by targeting nucleic acid modification pathways. QKY-613 promotes the selective incorporation of 6mdA (N6-methyldeoxyadenosine) into viral DNA, enhancing the phase separation potential of DNA, thereby increasing the activation of cGAS and strengthening host immune surveillance. In virus-infected mouse models, QKY-613 significantly reduced mortality in aged mice. QKY-613 holds promise for research on nucleic acid modification-based immune surveillance mechanisms .
    QKY-613
  • HY-116161A
    17-Phenyl trinor PGF2α isopropyl ester

    		Prostaglandin Receptor Endocrinology
    17-phenyl trinor PGF2α N-ethyl amide is an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug, sold under the Allergan trade name Bimatoprost.1 The N-ethyl amide prostaglandin prodrugs are converted to the active free acid more slowly than the analogous prostaglandin ester prodrugs such as latanoprost.2 This product is the isopropyl ester of the free acid prostaglandin which corresponds to Bimatoprost. The free acid, 17-phenyl trinor PGF2α, is a potent FP receptor agonist.3 In human and animal models of glaucoma, FP receptor agonist activity corresponds very closely with intraocular hypotensive activity. The 17-phenyl trinor PGF2α isopropyl ester derivative is examined for IOP-lowering activity during the development of latanoprost.4 At the dose of 3 μg/eye in the monkey, 17-phenyl trinor PGF2α isopropyl ester is the most potent analog tested in reducing IOP, lowering the IOP 1.3 mm Hg below the level achieved by latanoprost. However, this derivative is also significantly more irritating to the eye than latanoprost.
    17-Phenyl trinor PGF2α isopropyl ester
  • HY-134160
    5,6-Dihydro-5-Fluorouracil

    5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione; 5-Fluorodihydrouracil

    		 Others Cancer
    5,6-Dihydro-5-Fluorouracil (5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione) is the active metabolite of the thymidylate synthase inhibitor prodrug 5-fluorouracil (HY-90006), which is formed from 5-fluorouracil by dihydropyrimidine dehydrogenase (DPD). 5,6-Dihydro-5-Fluorouracil is cytotoxic to HaCaT keratinocytes (IC50=13.5 μM). Intravenous administration of 5,6-Dihydro-5-Fluorouracil (90 mg/kg/wk) in combination with 5-fluorouracil and the DPD inhibitor eniluracil (HY-10533) slows tumor growth in a rat colon cancer model.
    5,6-Dihydro-5-Fluorouracil
  • HY-147015
    HOE961

    		Orthopoxvirus Infection
    HOE961, the diacetate ester proagent of S2242, is active against respiratory cowpox virus infections, is orally active in infection models. Anti-orthopoxvirus activity .
    HOE961
  • HY-15334
    CEP-5214

    		VEGFR Cancer
    CEP-5214, derived from a new indenopyrrolocarbazole template, is a potent inhibitor of vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase. Structurally, it features optimal substitutions at positions 9 (ethoxymethyl) and 12 (hydroxypropyl) on the indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-one scaffold, leading to high potency against VEGF-R2 (IC50 8 nM). Compound 21 (CEP-5214) exhibits low-nanomolar inhibition of human VEGF-R tyrosine kinases (IC50 4 nM for VEGF-R2/KDR), with good selectivity over other kinases. The compound demonstrated significant cellular and in vivo antitumor activity across various models and advanced into phase I clinical trials as a water-soluble prodrug (CEP-7055) to enhance oral bioavailability .
    CEP-5214

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